scholarly journals Role of Biorelevant Dissolution Media in the Selection of Optimal Salt Forms of Oral Drugs: Maximizing the Gastrointestinal Solubility and in Vitro Activity of the Antimicrobial Molecule, Clofazimine

ACS Omega ◽  
2017 ◽  
Vol 2 (12) ◽  
pp. 8969-8981 ◽  
Author(s):  
Pauric Bannigan ◽  
Edel Durack ◽  
Conor Madden ◽  
Matteo Lusi ◽  
Sarah P. Hudson
Keyword(s):  
Vitro Activity ◽  
In Vitro Activity ◽  
Oral Drugs ◽  
Biorelevant Dissolution ◽  
Salt Forms ◽  
Biorelevant Dissolution Media ◽  
Selection Of

scholarly journals Selection of Retapamulin, a Novel Pleuromutilin for Topical Use

2006 ◽  
Vol 50 (11) ◽  
pp. 3882-3885 ◽  
Author(s):  
Stephen Rittenhouse ◽  
Sanjoy Biswas ◽  
John Broskey ◽  
Lynn McCloskey ◽  
Terrance Moore ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Streptococcus Pyogenes ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Postantibiotic Effect ◽  
Selection Of

ABSTRACT The in vitro activity of retapamulin was determined and compared to that of topical and community antibiotics. The MIC90s of retapamulin against Staphylococcus aureus and Streptococcus pyogenes were 0.12 μg/ml and 0.016 μg/ml, respectively. Retapamulin has a low propensity to select resistance and produces an in vitro postantibiotic effect.

scholarly journals Role of sugar chains in the in-vitro activity of recombinant human interleukin 5

1993 ◽  
Vol 211 (3) ◽  
pp. 903-908 ◽  
Author(s):  
Shiho KODAMA ◽  
Masafumi TSUJIMOTO ◽  
Nobuo TSURUOKA ◽  
Tsukasa SUGO ◽  
Tamao ENDO ◽  
...  
Keyword(s):  
Vitro Activity ◽  
In Vitro Activity ◽  
Interleukin 5 ◽  
Sugar Chains

scholarly journals Selection of a T7 promoter mutant with enhanced in vitro activity by a novel multi-copy bead display approach for in vitro evolution

2012 ◽  
Vol 41 (1) ◽  
pp. e29-e29 ◽  
Author(s):  
Siddhartha Paul ◽  
Alexander Stang ◽  
Klaus Lennartz ◽  
Matthias Tenbusch ◽  
Klaus Überla
Keyword(s):  
Vitro Activity ◽  
In Vitro Activity ◽  
T7 Promoter ◽  
In Vitro Evolution ◽  
Selection Of ◽  
Promoter Mutant

scholarly journals The effect of the branched-chain amino acids on the in-vitro activity of bovine intestinal alkaline phosphatase

2019 ◽  
Vol 44 (6) ◽  
pp. 632-636 ◽  
Author(s):  
Gary William Boyd ◽  
Marion Drew ◽  
Shannon Ward ◽  
Marianne Baird ◽  
Christopher Connaboy ◽  
...  
Keyword(s):  
Amino Acids ◽  
Alkaline Phosphatase ◽  
Branched Chain Amino Acids ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Intestinal Alkaline Phosphatase ◽  
Calf Intestinal Alkaline Phosphatase ◽  
Branched Chain

Branched-chain amino acids (BCAA) are used as nutritional support for patients with a range of conditions including liver cirrhosis and in-born errors of amino acid metabolism, and they are commonly used “sports” or exercise supplements. The effects of the BCAA on the in-vitro activity of calf intestinal alkaline phosphatase (EC. 3.1.3.1) were studied. All three BCAA were found to be uncompetitive inhibitors of the enzyme with L-leucine being the most potent ([Formula: see text] = 24.9 mmol/L) and L-valine, the least potent ([Formula: see text] = 37 mmol/L). Mixed BCAA are able to act in combination to inhibit the enzyme. Given the important role of intestinal alkaline phosphatase in gut homeostasis, these findings have potential implications for those taking high levels of BCAA as supplements.

scholarly journals Role of inorganic phosphate concentrations in in vitro activity of fosfomycin

2021 ◽  
Author(s):  
M. Ortiz-Padilla ◽  
I. Portillo-Calderón ◽  
N. Maldonado-Acosta ◽  
J.M. Rodríguez-Martínez ◽  
B. de Gregorio-Iaria ◽  
...  
Keyword(s):  
Inorganic Phosphate ◽  
Vitro Activity ◽  
In Vitro Activity

Role of Single-Electron Oxidation Potential and Lipophilicity in the Antiplasmodial in vitro Activity of Polyphenols: Comparison to Mammalian Cells

2008 ◽  
Vol 63 (5-6) ◽  
pp. 445-450 ◽  
Author(s):  
Philippe Grellier ◽  
Aušra Nemeikaitė-Čėnienė ◽  
Jonas Šarlauskas ◽  
Narimantas Čėnas
Keyword(s):  
Mammalian Cell ◽  
Mammalian Cells ◽  
Oxidation Potential ◽  
Vitro Activity ◽  
Antiplasmodial Activity ◽  
Cell Cytotoxicity ◽  
In Vitro Activity ◽  
Positive Dependence

In spite of extensive studies, the structure-activity relationships in the action of polyphenols against the malaria parasite Plasmodium falciparum are poorly understood so far. As the mammalian cell cytotoxicity of polyphenols shows a negative dependence on the potential of the phenoxyl radical/phenol redox couple (E27 ), due to the involvement of prooxidant events, and a positive dependence on the octanol/water distribution coefficient at pH 7.0 (log D), we examined the role of these parameters in their antiplasmodial in vitro activity. We found that the concentrations of hydroxybenzenes causing 50% inhibition of the growth of P. falciparum strain FcB1 (IC50) are described by the regression log IC50 (μm) = 0.36 + 1.81 E27 (V) - 0.10 log D [n = 11, r2 = 0.760, F(2.8) = 12.03]. The IC50 values of flavonoids (n = 5), comprising a separate less active series, did not depend on their E27 values, 0.33 V- 0.75 V. These findings were similar to the mammalian cell cytotoxicity data. However, the mammalian cell cytotoxicity of hydroxybenzenes showed more pronounced dependence on their E27 values [Δlog CL50 /ΔE27 = (6.9-5.1) V-1, where CL50 is the compound concentration for 50% cell survival] than on their antiplasmodial activity. Although it is unclear whether the prooxidant action is the main factor in the antiplasmodial action of polyphenols or not, our data showed that the ease of their oxidation (decrease in E27 ) may enhance their activity. On the other hand, the different sensitivity of the mammalian cell cytotoxicity and the antiplasmodial activity of the hydroxybenzenes to their E27 values implied that compounds with high oxidation potential may be used as relatively efficient antiplasmodial agents with low mammalian cell cytotoxicity.

Sign in / Sign up

Export Citation Format

Share Document